가수분해형 탄닌 1-desgalloylrugosin-F 에 의한 100kDa 세포질 포스포리파아제 A2 활성억제효과

• 영문명: Inhibition of 100kDa Cytosolic Phospholipase A2 by Hydrolysable Tannin, 1-desgalloylrugosin-F
• 발행기관: 대한약학회
• 저자명: 진미령(Mi Reyoung Chin) 신혜숙(Hye Sook Shin) 정광묵(Kwang Mook Jung) 강미선(Mi Sun Kang) 이민원(Min Won Lee) 김대경(Dae Kyong Kim)
• 간행물 정보: 『약학회지』제44권 제1호 (2000년), 47~51쪽, 전체 5쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2000.02.28

영문 초록

To examine whether DGRF inhibits cPLA2 activity in vitro, we purified a 100kDa cPLA2 enzyme from porcine spleen and performed an inhibition study at two concentrations of 5.0 and 50.0mcM 1-stearoyl-2-[1-14C]arachidonoyl-sn-glycero-3-phosphocholine as a substrate to rule out an apparent inhibition due to "substrate depletion". Here we reported that DGRF inhibited cPLA2 activity with ID50 of 3.2mcM and virtually complete inactivation of the enzyme occurred at 60mcM. Interaction experiment between enzyme protein and inhibitor by ultrafiltration method indicated that 1-desgalloylrugosin-F inactivates cPLA2 enzyme by an irreversible mechanism.

키워드

Cytosolic phospholipase A2 tannin 1-desgalloylrugosin-F inhibitor